Drug intelligence / Profile preview

YY2201

Development stage
Phase 1
Lead developer
Jiangsu Yayao Biotech
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Drug Delivery Systems
Administration
Oral
01

Overview

YY2201 is a highly potent and selective small-molecule inhibitor of ATR (ataxia telangiectasia and Rad3-related protein), a key kinase in the DNA damage response pathway. By inhibiting ATR, YY2201 induces DNA damage accumulation and apoptosis, particularly in cancer cells with deficiencies or mutations in other DNA damage response kinases, exploiting synthetic lethality. Preclinical studies have demonstrated that YY2201 efficiently inhibits tumor progression across a broad spectrum of cancer types both in vitro and in vivo, showing superior anticancer efficacy compared to AZD6738 (ceralasertib) in lung cancer xenograft models. The drug has favorable pharmacokinetic properties and safety profiles, with promising activity as monotherapy or combined with chemotherapy. It is being developed primarily for the treatment of advanced solid tumors[4][5][2].

Brand names
YY2201YY-2201YY 2201
Other names
YY2201YY-2201YY 2201
02

Targets

ATR (ATR serine/threonine kinase)

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